Serotonin Receptor Binding Affinities of Several Hallucinogenic Phenylalkylamine and N,N-Dimethyltryptamine Analogues
Richard A Glennon, Stephen M. Liebowitz, Elizabeth C. Mack
Journal of Medicinal Chemistry January 1, 1978 DOI: 10.1021/jm00206a022 (opens in new tab) via Elsevier
Summary
AI-generated from the abstractSeveral hallucinogenic compounds related to phenylalkylamine and N,N-dimethyltryptamine bind to serotonin (5-HT) receptors in rat stomach tissue. The most behaviorally potent analogues tested—DOB, DOM, and 5-methoxy-N,N-dimethyltryptamine—showed high binding affinities, with pA2 values of 7.35, 7.12, and 7.08, respectively.
Study at a glance
| Characteristics | In vitro study Peer reviewed |
|---|---|
| Population | Rat stomach fundus tissue |
| Citations | 35 |
| Key finding | The most behaviorally potent analogues DOB, DOM, and 5-methoxy-N,N-dimethyltryptamine had high affinities (pA2 = 7.35, 7.12, and 7.08) for 5-HT receptors in the rat stomach fundus model. |
Abstract
Hallucinogenic phenylalkylamine and N,N-dimethyltryptamine analogues are known to affect serotonergic systems both in vivo and in vitro. Using a rat stomach fundus model, the 5-HT receptor binding affinities of several of these analogues were determined and compared. The most behaviorally potent analogues examined, DOB, DOM, and 5-methoxy-N,N-dimethyltryptamine, were found to possess rather high affirmities (pA2 = 7.35, 7.12, and 7.08, respectively) for the 5-HT receptors of the model system.